CN103638008B - Artoxanthochromane在治疗皮肤癌药物中的应用 - Google Patents

Artoxanthochromane在治疗皮肤癌药物中的应用 Download PDF

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CN103638008B
CN103638008B CN201310634100.5A CN201310634100A CN103638008B CN 103638008 B CN103638008 B CN 103638008B CN 201310634100 A CN201310634100 A CN 201310634100A CN 103638008 B CN103638008 B CN 103638008B
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skin carcinoma
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CN103638008A (zh
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吴大军
李萍
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XI'AN LEKOU FUTAI BIOMEDICAL TECHNOLOGY Co.,Ltd.
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刘艳娇
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Abstract

本发明公开了Artoxanthochromane在制备治疗皮肤癌药物中的应用，属于药物新用途技术领域。本发明通过体外MTT抗肿瘤活性评价发现，Artoxanthochromane对人皮肤癌细胞株A431、HME1、A375和SK23的生长也具有显著的抑制作用。因此，Artoxanthochromane能用于制备抗皮肤癌药物，具有良好的开发应用前景。对于本发明涉及的Artoxanthochromane在制备治疗皮肤癌药物中的用途属于首次公开，而且其对于皮肤癌细胞的抑制活性强，具有显著的进步。

Description

Artoxanthochromane在治疗皮肤癌药物中的应用
技术领域
本发明涉及化合物Artoxanthochromane的新用途，尤其涉及Artoxanthochromane在制备治疗皮肤癌药物中的应用。
背景技术
癌症是对人类生命健康危害最大的疾病之一，每年都有大量的人死于癌症。抗癌药物的研发一直是药学研究的热点。抗肿瘤药物中有74%是天然产物或其衍生物，如紫杉醇及其衍生物就是目前临床上应用效果比较好的抗肿瘤药物。因此，从天然产物中寻找抗癌化合物或先导化合物具有重要的意义。
本发明涉及的化合物Artoxanthochromane是一个2013年发表（Horng-Huey Ko，et al.,A Novel MonoterpeneStilbene Adduct with a4,4-Dimethyl-2,3-diphenylchromaneSkeleton from Artocarpus xanthocarpus.chemistry&biodiversity,2013(10):1269-1275.）的新化合物，该化合物拥有全新的骨架类型，该化合物能清除氧自由基（Horng-Huey Ko，et al.,A Novel MonoterpeneStilbene Adduct with a4,4-Dimethyl-2,3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry&biodiversity,2013(10):1269-1275.），本发明涉及的Artoxanthochromane在制备治疗皮肤癌药物中的用途属于首次公开。
发明内容
本发明的目的在于根据现有Artoxanthochromane研究中未发现其具有抗皮肤癌活性的报道的现状，提供了Artoxanthochromane在制备抗皮肤癌药物中的应用。
所述化合物Artoxanthochromane,结构如式（Ⅰ）所示：
式（Ⅰ）
本发明通过体外MTT抗肿瘤活性评价发现，Artoxanthochromane对人皮肤癌细胞株A431、HME1、A375和SK23的生长也具有显著的抑制作用，抑制这4株细胞生长的IC50值分别为2.47±0.45μM、1.96±0.26μM、1.37±0.22μM和1.27±0.85μM。因此，Artoxanthochromane能用于制备抗皮肤癌药物，具有良好的开发应用前景。
对于本发明涉及的Artoxanthochromane在制备治疗皮肤癌药物中的用途属于首次公开，由于骨架类型属于全新的骨架类型，而且其对于皮肤癌细胞的抑制活性强，具备突出的实质性特点，同时用于皮肤癌的防治显然具有显著的进步。
以下通过实施例对本发明作进一步详细的说明，但本发明的保护范围不受具体实施例的任何限制，而是由权利要求加以限定。
具体实施方式
以下通过实施例对本发明作进一步详细的说明，但本发明的保护范围不受具体实施例的任何限制，而是由权利要求加以限定。
本发明所涉及化合物Artoxanthochromane的制备方法参见文献（Horng-Huey Ko，etal.,A Novel MonoterpeneStilbene Adduct with a4,4-Dimethyl-2,3-diphenylchromaneSkeleton from Artocarpus xanthocarpus.chemistry&biodiversity,2013(10):1269-1275.），按照上述方法制备化合物Artoxanthochromane。
实施例1：本发明所涉及化合物Artoxanthochromane片剂的制备：
取5克化合物Artoxanthochromane,加入糊精195克，混匀，常规压片制成1000片。
实施例2：本发明所涉及化合物Artoxanthochromane胶囊剂的制备：
取5克化合物Artoxanthochromane，加入淀粉195克，混匀，装胶囊制成1000粒。
下面通过药效学实验来进一步说明其药物活性。
实验例：采用MTT法评价化合物Artoxanthochromane对人皮肤癌细胞株的生长抑制作用
1.方法：处于生长对数期的细胞：人皮肤癌细胞株A431、HME1、A375和SK23（购买自中国科学院细胞库）以1.5×104浓度种于96孔板中。细胞培养24h贴壁后吸去原来的培养基。试验分为空白对照组、药物处理组。空白组更换含10%胎牛血清的1640培养基；药物处理组更换含浓度为100μM，50μM，10μM，1μM，0.1μM，0.01μM和0.001μM的Artoxanthochromane的培养基。培养48h后，加入浓度5mg/mL的MTT，继续放于CO2培养箱培养4h，然后沿着培养液上部吸去100μL上清，加入100μL DMSO，暗处放置10min，利用酶标仪（Sunrise公司产品）测定吸光值(波长570nm)，并根据吸光值计算细胞存活情况，每个处理设6个重复孔。细胞存活率(%)=ΔOD药物处理/ΔOD空白对照×100。
2.结果：Artoxanthochromane对人皮肤癌细胞株A431、HME1、A375和SK23的生长具有显著的抑制作用。该化合物抑制人皮肤癌细胞株A431、HME1、A375和SK23生长的IC50值分别为2.47±0.45μM、1.96±0.26μM、1.37±0.22μM和1.27±0.85μM。
由上述实施例表明，本发明的Artoxanthochromane对人皮肤癌细胞株A431、HME1、A375和SK23的生长具有很好的抑制作用。由此证明，本发明的Artoxanthochromane具有抗皮肤癌活性，能用于制备抗皮肤癌药物。

Claims (1)

1.Artoxanthochromane在制备治疗皮肤癌药物中的应用，所述化合物Artoxanthochromane结构如式(Ⅰ)所示：
CN201310634100.5A 2013-12-02 2013-12-02 Artoxanthochromane在治疗皮肤癌药物中的应用 Active CN103638008B (zh)

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Horng-Huey Ko等.a novel monoterpene-stilbene adduct with a 4,4-dimethyl-2,3-diphenylchromane skeleton from artocarpus xanthocarpus.《Chemistry Biodiversity》.2013,第10卷(第7期),1269-1275. *
自由基生物抗氧化与疾病;崔剑 等;《清华大学学报 自然科学版》;20001231;第40卷(第6期);9-12 *

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